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Nidufexor

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Chemical Structure| 1773489-72-7 同义名 : LMB763
CAS号 : 1773489-72-7
货号 : A615253
分子式 : C27H22ClN3O4
纯度 : 99%+
分子量 : 487.934
MDL号 : MFCD31657267
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(174.2 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The farnesoid X receptor (FXR) is a bile acid (BA)-activated nuclear receptor highly expressed in the liver, gall bladder, intestines, and kidney that regulates BA production, conjugation, and transport. Nidufexor is a novel FXR agonist for the treatment of nonalcoholic steatohepatitis (NASH). In adult male Wistar Han rats (age approximately 10 weeks), nidufexor exhibited moderate Cmax (4.5, 12.4, 28.1, 80.9, and 140.8 μM) and terminal elimination half-lives (t1/2; 3.9, 5.7, 6.3, 5.6, 6.3 h) following oral administration (3, 10, 30, 100, and 300 mg/kg). Following intravenous administration (mouse 3.0, rat 5.0 and, dog 0.5 mg/kg), nidufexor exhibited t1/2 values of 4.5, 4.4 and 6.8 h for mouse, rat and dog, respectively. While following oral administration (mouse 10, rat 10 and, dog 2 mg/kg), nidufexor exhibited t1/2 values of 3.5, 2.7 and 10.1 h for mouse, rat and dog, respectively. Nidufexor has advanced to Phase 2 human clinical trials in patients with NASH and diabetic nephropathy[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.20mL

10.25mL

2.05mL

1.02mL

20.49mL

4.10mL

2.05mL
参考文献

[1]Chianelli D, Rucker PV, Roland J, et al. Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis. J Med Chem. 2020 Apr 23;63(8):3868-3880